Patents Represented by Attorney, Agent or Law Firm Robert A. Silverman
  • Patent number: 5502210
    Abstract: The invention relates to intermediate compounds which are useful in the preparation of N-tert-butyl-decahydro-2- 2 (R)-hydroxy-4-phenyl-3(S)-phthalimidobutyl!-(4aS, 8aS)-isoquinoline-3(S)-carboxamide. The final products are suitable for the treatment of vital infections, such as those caused by HIV and other retroviruses.
    Type: Grant
    Filed: July 11, 1994
    Date of Patent: March 26, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Patent number: 5498367
    Abstract: A chiral dopant of the formula ##STR1## wherein ring A is 1,4-phenylene which is optionally substituted with one or more fluorine atoms, chlorine atoms, bromine atoms, cyano groups, or methyl groups, and in which one or two CH groups can be replaced by nitrogen, or is trans-1,4-cyclohexylene;Z is a single covalent bond, --CH.sub.2 CH.sub.2 --, --CH.sub.2 O-- or --OCH.sub.2 --;X.sup.1,X.sup.2,X.sup.3,X.sup.4 each independently are hydrogen or fluorine;R.sup.1 is hydrogen, is alkyl with 1 to 12 carbon atoms which is optionally substituted with one or more fluorine or chlorine atoms and in which one or two non-adjacent CH.sub.2 groups can be replaced by --O--, is alkenyl with 2 to 12 carbon atoms, which is optionally substituted with one or more fluorine or chlorine atoms and in which one or two non-adjacent CH.sub.2 groups can be replaced by --O--, is a group of the formula ##STR2## and when R.sup.1 is bonded to an aromatic ring, can also be fluorine, chlorine, cyano, CF.sub.3, OCHF.sub.2 or --OCF.sub.3 ;R.sup.
    Type: Grant
    Filed: February 17, 1995
    Date of Patent: March 12, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Guy Marck, Martin Schadt
  • Patent number: 5484551
    Abstract: Compounds containing a 4-[(E)-alk-2-enoyloxy]benzoate group and liquid crystalline mixtures which contain such compounds and the use of such compounds and, respectively, mixtures in electro-optical indicating devices.The compounds are of the formula ##STR1## wherein R.sup.1 is alkyl with 1 to 12 carbon atoms;X.sup.1, X.sup.3 each independently are halogen or hydrogen; andX.sup.2 is halogen or cyano.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: January 16, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephen Kelly, Martin Schadt
  • Patent number: 5476875
    Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: December 19, 1995
    Assignee: Hoffman-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
  • Patent number: 5474744
    Abstract: An automatic pipetting device comprising only one pipetting needle having a tip end and an open end. The device comprises a metering syringe having an outlet. The device also comprises a mechanism for cleaning the pipetting needle with a cleaning fluid when the pipetting needle is positioned in a cleaning position. The mechanism comprises a plunger pump, a second tube having a first end and a second end, a first valve, a second valve, and a third tube having a first end and a second end, the second end of the tubing immersed in a cleaning fluid. The second end of the first tube is in fluid communication with both the outlet of the metering syringe and the first valve. The first end of the second tube is in fluid communication with the first valve. The second end of the second tube is in fluid communication with both the plunger pump and the second valve. The first end of the third tube is in fluid communication with the second valve.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: December 12, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Erich Lerch
  • Patent number: 5472949
    Abstract: The invention relates to N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives which are useful as an agent for treating tumors, pharmaceutical compositions including the same, a method of treating tumors and a method of preparing N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives for treating tumors.Compounds of formula (I), ##STR1## wherein R.sup.1 is a saturated or unsaturated, straight or branched hydrocarbon radical wherein the number of carbon atoms in the longest straight chain of this hydrocarbon radical ranges from three to seven, or is a radical of the formula --(CH.sub.2)n--.sup.Y wherein Y is a cyclohexyl radical, a C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical and wherein when Y is a cyclohexyl radical n is an integer from 0 to 4, and when Y is C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical n is an integer from 2 to 4, and R.sup.2 is a hydrogen atom or a radical easily hydrolyzable under physiological conditions,or a hydrate or solvate thereof.
    Type: Grant
    Filed: December 14, 1993
    Date of Patent: December 5, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Motohiro Arasaki, Hideo Ishitsuka, Isami Kuruma, Masanori Miwa, Chikako Murasaki, Nobuo Shimma, Isao Umeda
  • Patent number: 5457219
    Abstract: Novel, racemic and optically active phosphorus compounds of the formula ##STR1## wherein R signifies lower alkyl or lower alkoxy and R.sup.1 represents lower alkyl, cycloalkyl or substituted phenyl, are described.The compounds of formula I are useful in the form of complexes with a metal of Group VIII as catalysts for asymmetric hydrogenations and for enantioselective hydrogen displacements in prochiral allylic systems.
    Type: Grant
    Filed: September 27, 1993
    Date of Patent: October 10, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Joseph Foricher, Rudolf Schmid
  • Patent number: 5457124
    Abstract: The invention relates to compounds selected from the group consisting of the formulas: ##STR1## wherein R.sup.2 and Ph are as described herein. These compounds are potent leukotriene B.sub.4 antagonists and are therefore useful in the treatment of inflammatory diseases.
    Type: Grant
    Filed: December 7, 1993
    Date of Patent: October 10, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Andrzej R. Daniewski, Ferdinand K. Lee, Keith A. Yagaloff
  • Patent number: 5451600
    Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, alkyl.sub.1-8, geminal alkyl.sub.1-3, unsubstituted or substituted aryl; X is alkylene, --CR.sub.1 .dbd.CR.sub.2 -- (E and/or Z), carbonyl, oxygen or sulfur, wherein one of R.sub.1 and R.sub.2 is alkyl.sub.1-3 and the other is hydrogen; Y is unsubstituted alkyl.sub.1-12 or substituted by one or more alkyl.sub.1-3 groups, or unsubstituted or substituted phenylalkyl .sub.1-3 ; or a salt thereof with a pharmaceutically acceptable base, are described.The compound of formula I are potent inhibitors of phospholipase A.sub.2 (PLA.sub.2) and are therefore useful in the treatment of inflammatory diseases, such as, psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary, myocardial ischemia and trauma induced inflammation, such as, spinal cord injury.
    Type: Grant
    Filed: April 19, 1994
    Date of Patent: September 19, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bruce L. Banner, Giuseppe F. Weber
  • Patent number: 5447657
    Abstract: The present invention provides compounds of the general formula: ##STR1## wherein R is an alkyl group with 1 to 12 carbon atoms or a group of the formula ##STR2## Ring A.sup.1 is 1,4-phenylene, which is unsubstituted or substituted with fluorine, pyridine-2,5-diyl or pyrimidine-2,5-diyl;Ring A.sup.2 is trans-1,4-cyclohexylene or trans-1,3-dioxane-2,5-diyl;R.sup.1 is an alkyl, alkenyl or alkoxyalkyl group with 1 to 12 and, respectively, 2 to 12 carbon atoms;X.sup.1 is fluorine, chlorine, bromine, trifluoromethyl, trifluoromethoxy or difluoromethoxy; andX.sup.2, X.sup.3 each independently are hydrogen or fluorine.The invention is also concerned with liquid crystal mixtures which contain these compounds and with the use of these compounds and mixtures for electro-optical purposes.
    Type: Grant
    Filed: March 8, 1994
    Date of Patent: September 5, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Schadt, Alois Villiger
  • Patent number: 5447658
    Abstract: Compounds of the general formula ##STR1## wherein R.sup.1 represents vinyl or straight-chain alkenyl with 3 to 7 carbon atoms,the manufacture of such compounds, liquid crystalline mixtures which contain such compounds as well as the use of such compounds for electro-optical purposes.
    Type: Grant
    Filed: June 17, 1994
    Date of Patent: September 5, 1995
    Assignees: Hoffman-La Roche Inc., Dainipppon Ink and Chemicals, Inc.
    Inventors: Richard Buchecker, Teodor Lukac, Martin Schadt, Haruyoshi Takatsu, Alois Villiger
  • Patent number: 5447953
    Abstract: The use of biomasses obtained in the fermentative production of lipase inhibitors, especially lipstatin, for the preparation of foodstuffs, feedstuffs, food additives, feed additives, feed supplements, medicinal feed premixes or medicaments for oral administration, are described.
    Type: Grant
    Filed: June 17, 1994
    Date of Patent: September 5, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Dorothea Isler, Walter Rehm, Erich Widmer
  • Patent number: 5434186
    Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: July 18, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff
  • Patent number: 5430191
    Abstract: Novel racemic and optically active phosphorus compounds of the formula ##STR1## wherein R signifies hydroxy or a protected hydroxy group, R.sup.1 represents hydroxy, a protected hydroxy group or lower alkoxy and R.sup.2 represents lower alkyl, cycloalkyl, aryl or together with the phosphorus atom a group of the formula are described. The compounds of formula I are useful in the form of complexes with a metal of Group VIII as catalysts for asymmetric hydrogenations and for enantioselective hydrogen displacements in parochial, allylic systems.
    Type: Grant
    Filed: September 27, 1993
    Date of Patent: July 4, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Joseph Foricher, Rudolf Schmid
  • Patent number: 5428029
    Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, X is H.sub.2 or .dbd.CH.sub.2, and the 23,24-double bond is E or Z, are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of tumors such as breast cancer, as agents for the treatment of neoplastic diseases such as leukemia, and as agents for the treatment of sebaceous gland diseases such as acne and seborrheic dermatitis.
    Type: Grant
    Filed: November 24, 1993
    Date of Patent: June 27, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thomas I. Doran, Bernard M. Hennessy, John A. McLane, Giacomo Pizzolato, Farhad Sedarati, Milan R. Uskokovic
  • Patent number: 5420129
    Abstract: The invention is concerned with novel sulphonamides and their use as medicaments. In particular, the invention is concerned with compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, lower-alkyl, lower-alkoxy, lower-alkylthio, halogen or trifluoromethyl;R.sup.2 is hydrogen, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or --OCH.sub.2 COOR.sup.9 ;R.sup.3 is hydrogen, lower-alkyl, halogen, lower-alkylthio, trifluoromethyl, lower-alkoxy or trifluoromethoxy;R.sup.2 and R.sup.3 together are butadienyl, methylenedioxy, ethylenedioxy or isopropylidenedioxy;R.sup.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: May 30, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 5413734
    Abstract: Compounds of the formula ##STR1## wherein ring A is trans-1,4-cyclohexylene, 1,4-phenylene, pyrimidine-2,5-diyl or trans-1,3-dioxane-2,5-diyl; n is either 0 or 1; ring B stands for 1,4-phenylene or trans-1,4-cyclohexylene; and R.sup.1 is 3E-alkenyl or on a saturated ring also 1E-alkenyl, their manufacture, liquid crystalline mixtures which contain these compounds as well as their use for electro-optical purposes.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: May 9, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Martin Schadt
  • Patent number: 5405854
    Abstract: Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.
    Type: Grant
    Filed: February 24, 1993
    Date of Patent: April 11, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, Gerard Schmid
  • Patent number: 5401733
    Abstract: The invention relates to the compounds 1,25-dihydroxy-16-ene-24-oxo-cholecalciferol and 1,24,25-trihydroxy-16-ene-cholecalciferol which stimulate differentiation of HL-60 cells, rendering them useful as an agent for the treatment of neoplastic diseases such as leukemia, and also decrease proliferation of human keratinocytes, rendering them useful as an agent for the treatment of hyperproliferative disorders of the skin such as psoriasis.
    Type: Grant
    Filed: October 1, 1993
    Date of Patent: March 28, 1995
    Assignees: Hoffmann-La Roche Inc., Satyanarayama G. Reddy
    Inventors: John A. McLane, Satyanarayama G. Reddy, Milan R. Uskokovic
  • Patent number: 5393458
    Abstract: Compounds of the general formula ##STR1## wherein R.sup.1 signifies alkyl or alkenyl with 1 to 12 and, respectively, 2 to 12 carbon atoms, which is unsubstituted or mono- or multiply-substituted with halogen and in which one methylene group can be replaced by --O--;R.sup.2 signifies alkyl or alkenyl with 1 to 12 and, respectively, 2 to 12 carbon atoms, which is unsubstituted or mono- or multiply-substituted with halogen and in which one or more methylene groups can be replaced by --O-- and/or --COO-- or --OOC--;Z.sup.1 signifies a single covalent bond or --CH.sub.2 CH.sub.2 --;A.sup.1, A.sup.2 each independently represent 1,4-phenylene, which is unsubstituted or mono- or multiply-substituted with halogen, or pyridine-2,5-diyl or pyrimidine-2,5-diyl;A.sup.3 represents 1,4-phenylene, which is unsubstituted or mono- or multiply-substituted with halogen, or pyridine-2,5-diyl, pyrimidine-2,5-diyl or trans-1,4-cyclohexylene;n is 0 or 1;with the proviso that at least one of rings A.sup.1, A.sup.2 or A.sup.
    Type: Grant
    Filed: March 29, 1994
    Date of Patent: February 28, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Stephen Kelly